e-Drug3D

1991

M RIPRETINIB

INN
RIPRETINIB

(is an active metabolite)

cas 1442473-09-7

CLASS

ANTINEOPLASTIC
KIT PROTO-ONCOGENE RECEPTOR TYROSINE KINASE INHIBITOR
PLATELET DERIVED GROWTH FACTOR RECEPTOR A (PDGFRA) INHIBITOR
TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR (GIST)
INHIBITS PDGFRB, TIE2, VEGFR2, AND BRAF

ROUTE (list)

-

ATC code

L01EX19

PK parameters

Tmax 15.6 HOUR
Cmax 1.62 MICROMOLAR
VD 507 LITER
Cl 17.5 LITER / HOUR
PPB 99.8 PERCENT
t1/2 17.8 HOUR

Target

TARGET PROTO-ONCOGENE RECEPTOR TYROSINE KINASE (KIT)

Mast,stem cell growth factor receptor Kit UNIPROT P10721 KIT

Platelet-derived growth factor receptor alpha UNIPROT P16234 PDGFRA

Download SDF file

Urea, N-[5-(7-amino-1-ethyl-1,2-dihydro-2-oxo-1,6-naphthyridin-3-yl)-4-bromo-2-fluorophenyl]-N'-phenyl-

Formula:
C23H19BrFN5O2

Calculated chemical properties:

MW 496.33
NB_atoms 32
XLogP 5.21
PSA 90.966
NB_HD 4
NB_HA 7
fsp3 0.09
Lipinski(0=no;1=yes) 0

FDA
-

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1990

RIPRETINIB

INN
RIPRETINIB

(has an active metabolite)

cas 1442472-39-0

CLASS

ANTINEOPLASTIC
KIT PROTO-ONCOGENE RECEPTOR TYROSINE KINASE INHIBITOR
PLATELET DERIVED GROWTH FACTOR RECEPTOR A (PDGFRA) INHIBITOR
TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR (GIST)
INHIBITS PDGFRB, TIE2, VEGFR2, AND BRAF

ROUTE (list)

ORAL

ATC code

L01EX19

PK parameters

Tmax 4 HOUR
Cmax 1.49 MICROMOLAR
VD 307 LITER
Cl 15.3 LITER / HOUR
PPB 99.8 PERCENT
t1/2 14.8 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER

Target

TARGET PROTO-ONCOGENE RECEPTOR TYROSINE KINASE (KIT)

Mast,stem cell growth factor receptor Kit UNIPROT P10721 KIT

Platelet-derived growth factor receptor alpha UNIPROT P16234 PDGFRA

Download SDF file

Urea, N-[4-bromo-5-[1-ethyl-1,2-dihydro-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-N'-phenyl-

Formula:
C24H21BrFN5O2

Calculated chemical properties:

MW 510.36
NB_atoms 33
XLogP 5.67
PSA 80.243
NB_HD 3
NB_HA 7
fsp3 0.12
Lipinski(0=no;1=yes) 0

FDA
NDA 213973 (label) INN (RIPRETINIB) QINLOCK (DECIPHERA PHARMS) APPROVAL= AP YEAR= 2020 NEWMOLECULARENTITY

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL